2170136-02-2
Chemical Structure
(Rac)-GSK-3484862
Synonym(s): GSK3482364
- CAS No.: 2170136-02-2
- Formula:C19H19N5OS
- Molecular Weight:365.45
IUPAC Name: 2-((3,5-dicyano-6-(dimethylamino)-4-ethylpyridin-2-yl)thio)-2-phenylacetamide
InChIKey: KIEQQZZDWUNUQK-UHFFFAOYSA-N
SMILES: O=C(N)C(SC1=NC(N(C)C)=C(C#N)C(CC)=C1C#N)C2=CC=CC=C2
Biological Activity: (Rac)-GSK-3484862 (GSK3482364) is a selective, orally active, reversible DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 of 0.4 μM. (Rac)-GSK-3484862 inhibits the methyltransferase activity of DNMT1 independently of DNA incorporation, reduces global DNA methylation levels, and relieves the transcriptional repression of HBG1 and HBG2 genes. (Rac)-GSK-3484862 increases fetal hemoglobin levels and the proportion of red blood cells expressing fetal hemoglobin in erythroid progenitor cells and a transgenic mouse model of sickle cell disease. (Rac)-GSK-3484862 can be used in studies related to sickle cell disease[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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(Rac)-GSK-3484862 | 98.76% | (Rac)-GSK-3484862 (GSK3482364) is a selective, orally active, reversible DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 of 0.4 μM. (Rac)-GSK-3484862 inhibits the methyltransferase activity of DNMT1 independently of DNA incorporation, reduces global DNA methylation levels, and relieves the transcriptional repression of HBG1 and HBG2 genes. (Rac)-GSK-3484862 increases fetal hemoglobin levels and the proportion of red blood cells expressing fetal hemoglobin in erythroid progenitor cells and a transgenic mouse model of sickle cell disease. (Rac)-GSK-3484862 can be used in studies related to sickle cell disease. | ||||||||||||||||||||
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References
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[1]. Gilmartin AG, et al. In vitro and in vivo induction of fetal hemoglobin with a reversible and selective DNMT1 inhibitor. Haematologica. 2021 Jul 1;106(7):1979-1987.
[Content Brief] - [2]. Ala C, et al. Discovery of potent DNMT1 inhibitors against sickle cell disease using structural-based virtual screening, MM-GBSA and molecular dynamics simulation-based approaches. Journal of biomolecular structure & dynamics. 2024;42(1):261-273. [Content Brief]
